Table 3

Pharmacological characterization of β-adrenoceptor subtypes

Potency orderISO > E = NEISO > E > NEISO = NE > E?
Selective agonistsNE3-a TerbutalineCGP 121773-c CGP 121773-c
Xamoterol3-a 3-b SalbutamolCL 3162433-d RO 363 (μM)
RO 363 (nM)3-a 3-b ProcaterolBRL 373443-d
Selective antagonistsCGP 20712A (8.5–9.3)ICI 118,551Bupranolol3-c Bupranolol3-c
Betaxol (8.5)(8.3–9.2)(6.9–7.3)(6.4–7.3)
Atenolol (7.6)SR 59230A
Bisoprolol (8.1–8.8)(7.5–8.8)
  • ISO, isoprenaline; NE, noradrenaline; E, adrenaline. Drug affinities (numbers in parentheses) are expressed as −logK i or −log K B values. Adapted from Alexander and Peters (1999), Bylund et al. (1998), Brodde (1997),Kaumann and Molenaar (1997), Manara et al. (1996), Molenaar et al. (1997).

  • 3-a Selective relative to β2-adrenoceptors.

  • 3-b In some tissues, partial agonists.

  • 3-c Antagonists with high affinity at β1- and β2-adrenoceptors.

  • 3-d Have higher intrinsic activity at rodent β3-adrenoceptors than at human β3-adrenoceptors.